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Purity: ≥98%
DT-061 (also known as DT061; SMAP) is a novel, potent and orally bioavailable activator of PP2A (protein phosphatase 2A) with anticancer effects. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis. Treatment with DT-061, in combination with the MEK inhibitor AZD6244, resulted in suppression of both p-AKT and MYC, as well as tumor regression in two KRAS-driven lung cancer mouse models. DT-061 therapy also abrogated MYC-driven tumorigenesis.
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| ln Vivo |
DT-061 (5 mg/kg, oral gavage, 4 weeks) inhibits the growth of H358 or H441 xenografts as a single agent. Furthermore, there is a considerable increase in efficiency when DT-061 and AZD6244 are combined[1].
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| Animal Protocol |
Animal/Disease Models: 6 - to 8weeks old male BALB/c nu/nu (nude) mice injected with H441 cells (5 × 106)[1].
Doses: 5 mg/kg. Route of Administration: po (oral gavage) for 4 weeks. Experimental Results: demonstrated activity in inhibiting tumor growth. |
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| References |
| Molecular Formula |
C25H23F3N2O5S
|
|---|---|
| Molecular Weight |
520.5207
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| Exact Mass |
520.127
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| CAS # |
1809427-19-7
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| Related CAS # |
(1S,2S,3R)-DT-061;1809427-20-0
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| PubChem CID |
91885558
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
824
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])OC(F)(F)F)(N([H])[C@]1([H])C([H])([H])C([H])([H])C([H])([H])[C@@]([H])([C@@]1([H])O[H])N1C2=C([H])C([H])=C([H])C([H])=C2OC2=C([H])C([H])=C([H])C([H])=C12)(=O)=O
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| InChi Key |
WGKGADVPRVLHHZ-ZHRMCQFGSA-N
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| InChi Code |
InChI=1S/C25H23F3N2O5S/c26-25(27,28)35-16-12-14-17(15-13-16)36(32,33)29-18-6-5-9-21(24(18)31)30-19-7-1-3-10-22(19)34-23-11-4-2-8-20(23)30/h1-4,7-8,10-15,18,21,24,29,31H,5-6,9H2/t18-,21+,24+/m1/s1
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| Chemical Name |
N-((1R,2R,3S)-2-hydroxy-3-(10H-phenoxazin-10-yl)cyclohexyl)-4-(trifluoromethoxy)benzenesulfonamide
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| Synonyms |
DT 061; DT61; SMAP; DT-061; DT061; DT-61; DT 61
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~240.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.00 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9212 mL | 9.6058 mL | 19.2116 mL | |
| 5 mM | 0.3842 mL | 1.9212 mL | 3.8423 mL | |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9212 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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